Solubility-physicochemical-thermodynamic theory of penetration enhancer mechanism of action.

Abstract:

:The hypothesis for the investigation was that the overall mechanism of action of skin penetration enhancers is best explained by the Solubility-Physicochemical-Thermodynamic (SPT) theory. To our knowledge, this is the first report of the application of SPT theory in transdermal/topical/enhancer research. The SPT theory puts forward the concept that the mode of action of enhancers is related to solubility parameters, physicochemical interactions and thermodynamic activity. This paper discusses these concepts by using experimentally derived permeation data, various physicochemical and solubility parameters (ingredient active gap (IAG), ingredient skin gap (ISG), solubility of active in the formulation (SolV) and the formulation solubility in the skin (SolS)) generated by using FFE (Formulating for Efficacy™ - ACT Solutions Corp) software. These studies suggest that there is an inverse relationship between measured flux and IAG values given that there is an optimum ingredient skin gap, SolV and SolS ratio. The study demonstrated that the flux is actually proportional to a gradient of thermodynamic activity rather than the concentration and maximum skin penetration and deposition can be achieved when the drug is at its highest thermodynamic activity.

journal_name

Int J Pharm

authors

Haq A,Chandler M,Michniak-Kohn B

doi

10.1016/j.ijpharm.2019.118920

subject

Has Abstract

pub_date

2020-02-15 00:00:00

pages

118920

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(19)30965-2

journal_volume

575

pub_type

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